Dosing & Uses
Dosage Forms & Strengths
tablet
- 650mg
Menorrhagia
Indicated for the treatment of cyclic heavy menstrual bleeding
1300 mg PO TID for up to 5 days during menstruation
Renal impairment
- SCr >1.4 mg/dL and ≤2.8 mg/dL: 1300 mg PO BID
- SCr >2.8 mg/dL and ≤5.7 mg/dL: 1300 mg PO qDay
- SCr >5.7 mg/dL: 650 mg PO qDay
- Each regimen listed above may be administered for up to 5 days during menstruation
Hepatic impairment
- Dose adjustments not necessary
Hereditary Angioedema (Off-label)
Long term prophylaxis: 1000-1500 mg PO q8-12hr; reduce dose to 500 mg/dose PO qDay or q12hr when frequency of attacks reduces
Short term prophylaxis: 75 mg/kg/day PO divided q8-12hr for 5 days before and after the event
Treatment of acute HAE attack: 25 mg/kg/dose PO/IV; not to exceed 1000 mg/dose q3-4hr; not to exceed 75 mg/kg/day or 1000 mg PO q6hr for 48 hr
Cone Biopsy (Off-label)
1000-1500 mg q8-12hr x12 days postop
Epistaxis (Off-label)
1000-1500 mg q8-12hr x10 days
Hyphema (Off-label)
1000-1500 mg q8-12hr x7 days
Hereditary Angioedema (Off-label)
1000-1500 mg PO BID/TID
Administration
May take with or without food
Swallow whole, do not chew, break, or crush
Indicated for women of reproductive age and is not intended for use in premenarcheal girls
Based on a pharmacokinetic study in 20 adolescent females, aged 12-16 years, no dose adjustment is needed in the adolescent population
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (3)
- dienogest/estradiol valerate
tranexamic acid oral, dienogest/estradiol valerate. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk.
- ethinylestradiol
tranexamic acid oral, ethinylestradiol. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk.
- mestranol
tranexamic acid oral, mestranol. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk .
Serious - Use Alternative (4)
- anti-inhibitor coagulant complex
tranexamic acid oral, anti-inhibitor coagulant complex. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.
anti-inhibitor coagulant complex, tranexamic acid oral. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration ma. - Factor IX
tranexamic acid oral, Factor IX. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.
- Factor IX complex
tranexamic acid oral, Factor IX complex. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.
- Factor IX, recombinant
tranexamic acid oral, Factor IX, recombinant. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.
Monitor Closely (5)
- alteplase
tranexamic acid oral, alteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
- defibrotide
tranexamic acid oral decreases effects of defibrotide by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Defibrotide may diminish effects of thrombolytic agents. Consider therapy modification.
- reteplase
tranexamic acid oral, reteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
- tenecteplase
tranexamic acid oral, tenecteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.
- tretinoin
tranexamic acid oral, tretinoin. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration may increase procoagulant effect.
Minor (0)
Adverse Effects
>10%
Headache (50.4%)
Nasal and sinus symptoms (25.4%)
Back pain (20.7%)
Abdominal pain (19.8%)
Musculoskeletal pain (11.2%)
1-10%
Arthralgia (6.9%)
Muscle cramps and spasms (5.8%)
Migraine (6%)
Anemia (5.6%)
Fatigue (5.2%)
Postmarketing Reports
Nausea, vomiting, and diarrhea
Allergic skin reactions
Anaphylactic shock and anaphylactoid reactions
Thromboembolic events (eg, DVT, pulmonary embolism, cerebral thrombosis, acute renal cortical necrosis, and central retinal artery and vein obstruction); cases have been associated with concomitant use of combination hormonal contraceptives Impaired color vision and other visual disturbances
Dizziness
Warnings
Contraindications
Hypersensitivity
Women using combination hormonal contraceptives
Active thromboembolic disease (eg, DVT, pulmonary embolism, or cerebral thrombosis)
History of thrombosis or thromboembolism, including retinal vein or artery occlusion
Intrinsic risk of thrombosis or thromboembolism (eg, thrombogenic valvular disease, thrombogenic cardiac rhythm disease, or hypercoagulopathy)
Cautions
Increased risk for thrombosis when coadministered with combination oral contraceptive (see Contraindications), Factor IX complex concentrates, anti-inhibitor coagulant concentrates, or oral tretinoin
Venous and arterial thrombosis or thromboembolism, as well as cases of retinal artery and retinal vein occlusions, have been reported
Severe allergic reaction reported; anaphylactic shock reported with IV product
May cause cerebral edema and cerebral infarction in women with subarachnoid hemorrhage
Ligneous conjunctivitis reported
Pregnancy & Lactation
Pregnancy
Not indicated for use in pregnant women; there are no available data on use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes; tranexamic acid crosses the placenta; animal reproduction studies have not identified adverse developmental outcomes with oral administration of tranexamic acid to pregnant rats at doses up to 4 times the recommended human dose
Lactation
Tranexamic acid is present in the mother’s milk at a concentration of about one hundredth of the corresponding serum concentration; the amount of tranexamic acid a nursing infant would absorb is unknown; there are no adequate data on effects of tranexamic acid on breastfed infant or on milk production; the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on breast-fed child from therapy or from underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Antifibrinolytic; synthetic lysine amino acid derivative, which diminishes the dissolution of hemostatic fibrin by plasmin In the presence of tranexamic acid, the lysine receptor binding sites of plasmin for fibrin are occupied, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin’s matrix structure
Absorption
Bioavailability: 45%
Peak plasma time: 2.5 hr
Peak plasma concentration: 16.41 mcg/mL (steady-state)
AUC: 80.19 mcg•hr/mL
Distribution
Protein bound: 3%
Vd: 0.18 L/kg (initial); 0.39 L/kg (steady-state)
Metabolism
Small fraction is metabolized
Elimination
Half-life: 11.08 hr
Eliminated by urinary excretion primarily via glomerular filtration
Excretion: 90% urine; >95% of the dose excreted unchanged
Images
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
